新型喹诺酮WIN-57273对金黄色葡萄球菌的相对β-内酰胺酶和转肽酶抑制活性
Relative beta-lactamase- and transpeptidase-inhibitory activities of the new quinolone WIN-57273 in Staphylococcus aureus.
作者信息
Furet Y X, Lucain C, Pechère J C
机构信息
Département de Microbiologie Médicale, Centre Médical Universitaire, Geneva, Switzerland.
出版信息
Antimicrob Agents Chemother. 1992 Apr;36(4):894-7. doi: 10.1128/AAC.36.4.894.
Abstract
The new quinolone WIN-57273 was shown to inhibit Staphylococcus aureus beta-lactamase activity noncompetitively in vitro with an apparent Ki value of 0.5 mM. MICs of penicillin G for a highly quinolone-resistant, beta-lactamase-negative strain in the presence of exogenous beta-lactamase decreased considerably when subinhibitory concentrations of WIN-57273 were added. Furthermore, the attachment transpeptidase reaction, investigated on whole cells of S. aureus, was impeded by WIN-57273 concentrations of greater than or equal to 30 microM. While these interactions suggest a novel mechanism of action for this compound, they are probably not relevant to the overall antibacterial potency of WIN-57273.
摘要
新型喹诺酮WIN-57273在体外被证明能以非竞争性方式抑制金黄色葡萄球菌β-内酰胺酶活性，其表观抑制常数（Ki）值为0.5 mM。当添加亚抑制浓度的WIN-57273时，在存在外源性β-内酰胺酶的情况下，青霉素G对高度耐喹诺酮、β-内酰胺酶阴性菌株的最低抑菌浓度（MIC）显著降低。此外，在金黄色葡萄球菌全细胞上研究的转肽酶连接反应，在WIN-57273浓度大于或等于30 microM时受到阻碍。虽然这些相互作用表明该化合物有新的作用机制，但它们可能与WIN-57273的整体抗菌效力无关。
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